Assay Detail
Binding
CHEMBL1039906
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 4.47 | 5.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL565829 | — | — | 1 | 5.01 |
| CHEMBL567916 | — | — | 1 | 4.41 |
| CHEMBL576256 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL565829 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL567916 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL576256 | — | IC50 | = | 100000.0 | nM | 4.00 |